An outline of desensitization in pentameric ligand-gated ion channel receptors

Keramidas, Angelo and Lynch, Joseph W. (2012) An outline of desensitization in pentameric ligand-gated ion channel receptors. Cellular and Molecular Life Sciences, 70 7: 1241-1253. doi:10.1007/s00018-012-1133-z

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Author Keramidas, Angelo
Lynch, Joseph W.
Title An outline of desensitization in pentameric ligand-gated ion channel receptors
Journal name Cellular and Molecular Life Sciences   Check publisher's open access policy
ISSN 1420-682X
Publication date 2012-08-30
Year available 2013
Sub-type Article (original research)
DOI 10.1007/s00018-012-1133-z
Open Access Status Not Open Access
Volume 70
Issue 7
Start page 1241
End page 1253
Total pages 13
Place of publication Basel, Switzerland
Publisher Birkhaeuser Verlag AG
Language eng
Abstract Pentameric ligand-gated ion channel (pLGIC) receptors exhibit desensitization, the progressive reduction in ionic flux in the prolonged presence of agonist. Despite its pathophysiological importance and the fact that it was first described over half a century ago, surprisingly little is known about the structural basis of desensitization in this receptor family. Here, we explain how desensitization is defined using functional criteria. We then review recent progress into reconciling the structural and functional basis of this phenomenon. The extracellular–transmembrane domain interface is a key locus. Activation is well known to involve conformational changes at this interface, and several lines of evidence suggest that desensitization involves a distinct conformational change here that is incompatible with activation. However, major questions remain unresolved, including the structural basis of the desensitization-induced agonist affinity increase and the mechanism of pore closure during desensitization.
Keyword Single channel kinetics
Ligand-gated ion channel
Q-Index Code C1
Q-Index Status Confirmed Code
Institutional Status UQ
Additional Notes Published online: 31 August 2012.

Document type: Journal Article
Sub-type: Article (original research)
Collections: Queensland Brain Institute Publications
Official 2013 Collection
School of Biomedical Sciences Publications
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Citation counts: TR Web of Science Citation Count  Cited 15 times in Thomson Reuters Web of Science Article | Citations
Scopus Citation Count Cited 15 times in Scopus Article | Citations
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Created: Fri, 09 Nov 2012, 02:57:43 EST by Debra McMurtrie on behalf of Queensland Brain Institute